Expiration date: 01/2025

The composition and form of issue:

Tablets. 1 tablet contains terbinafine hydrochloride 281,31 mg (corresponds to 250 mg of terbinafine) 

excipients: microcrystalline cellulose sodium starch of glycolate starch Pregelatinised magnesium stearate silica colloidal anhydrous 

in blistere 4 PCs the paper cartons 4, 5, 7 or 10 blisters.

Cream. 1 g contains terbinafine hydrochloride 10 mg

excipients: cetyl alcohol stearyl alcohol cetyl palmitate benzyl alcohol sorbitan monostearate isopropyl myristate sodium hydroxide Polysorbate 60 purified water 

in tubes of 10 g in a cardboard bundle 1 tuba.

Description pharmaceutical form:

Tablets: white or almost white, round, biconvex with a smooth surface on both sides.

Cream: homogeneous, white or almost white.

Pharmacokinetics:

In oral administration is well absorbed. Using 0.8 h absorbed half the dose in 4-6 hours half of the dose distributed in the body. After 1-2 hours after ingestion of a single dose of 250 mg Cmax in the blood plasma reaches the value of 0.97 µg/ml. Bioavailability of 80%. Eating does not affect the bioavailability of terbinafine.

The local application, absorption of < 5%, it has little systemic effect.

Terbinafine is intensively bound to blood plasma proteins (99%), spreads rapidly in tissues, penetrates into the dermal layer of the skin and the nail plate. Penetrates the sebum and accumulates in high concentrations in hair follicles, hair, skin and in the subcutaneous tissue. After a few weeks of treatment accumulates in the nails in concentrations, provides fungicidal effect. T1/2 is 11 to 18 h, T1/2 terminal phase — 200-400 h

Biotransformiroetsa in the liver to inactive metabolites 80% of the dose is excreted in the urine as metabolites, the remainder 20% with feces. Not cumulates in the body. The patients ' age did not affect the farmakokinetiku terbinafine, however, the elimination may be reduced in patients with lesions of the liver or kidneys, resulting in high concentrations of terbinafine in the blood.

Excreted in breast milk.

Description pharmacological action:

Terbinafine belongs to the group of allylamines has a broad spectrum of antifungal activity. In low concentrations has a fungicidal effect on dermatophytes Trychophyton (T. rubrum, T. mentagrophytes,T. tonsurans, T. verrucosum, T. violaceum), Microsporum canis, Epidermophyton floccosum, fungi (e.g. Aspergillus, Cladosporium, Scopulariopsis brevicaulis), yeast fungi, mainly Candida albicans, and certain dimorphic fungi. The fungi Candida and its mycelial form has, depending on the species of mushroom, fungicidal or fungistatic.

Terbinafine violates the early stage of the biosynthesis of the main components of the cell membrane of the fungus ergosterol by inhibiting enzyme squalene epoxidase. Skvalenepoksidazu is not associated with the cytochrome P450 system (SUR450), therefore, terbinafine does not affect the metabolism of hormones and drugs, the metabolism which is associated with SUR450.

When administered orally accumulate in skin, nails and hair in amounts that have a fungicidal effect. Systemic treatment of multi-colored lichen, caused by Malassezia furfur, is inefficient.

Indications:

Tablets:

• mycosis of the scalp (trichophytosis, microsporia)
  
• mycoses of the skin and nails caused Trychophyton (T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum (M. canis, M. gypseum) and Epidermophyton floccosum
  
• the onychomycosis
  
• heavy, common ringworm of the smooth skin of the trunk and extremities, requiring systemic treatment
  
• candidiasis of the skin and mucous membranes.
  

Cream (prevention and treatment):

• fungal infections of the skin, including mycosis of the feet ("fungus" foot), groin the athlete's (tinea cruris), fungal defeat smooth skin (tinea corporis) caused by Trichophyton (including T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum
  
• yeast infections of the skin, mainly those that are called come from Candida (e.g. Candida albicans), in particular diaper rash
  
• pityriasis versicolor (Pityriasis versicolor), called Pityrosporum orbiculare (also called Malassezia furfur).
  

Contraindications:

Hypersensitivity to any component of the drug

Tablets:

• children up to age 2 years, because no sufficient data on the use of drugs children with body weight less than 12 kg
  
• pregnancy
  
• the lactation period.
  

With caution:

Tablets:

• liver and/or kidney failure
  
• alcoholism
  
• tumors
  
• diseases of metabolism
  
• diseases of the blood
  
• pathology of the vessels of the extremities
  
• psoriasis.
  

Cream:

• liver and/or kidney failure
  
• alcoholism
  
• tumors
  
• diseases of metabolism
  
• inhibition of bone marrow hematopoiesis
  
• occlusive vascular disease of the limbs
  
• children up to age 12 years (the lack of sufficient clinical experience).
  

Application of pregnancy and breast-feeding:

Pills

Contraindicated during pregnancy. At the time of treatment should stop breastfeeding.

Cream

In experimental studies teratogenic properties of terbinafine have been identified. So far not reported about any defects in the application Aktifin. However, because clinical experiences with Activin in pregnant women is very limited, it should be used only on strict conditions.

Terbinafine is excreted in breast milk. However, in the case of a nursing mother Azifine cream absorbed through the skin a small amount of active substance, therefore, adverse effects on the baby are unlikely.

Side effects:

Tablets: side effects are usually moderate and mild severity and are temporary in nature.

On the part of the digestive system: often — feeling of a full stomach, indigestion, nausea, loss of appetite, abdominal pain, diarrhea, not often — violation of taste perception, including taste loss, which recovers within a few weeks after cessation of treatment rarely cholestasis, jaundice, hepatitis, asymptomatic increase in transaminases of the liver. Despite the lack of evidence of a causal relationship of these disorders with taking terbinafine, in the case of the development of hepatobiliary dysfunction treatment Aquifina should be discontinued.

CNS: rarely — paresthesia, hypoesthesia, dizziness, rarely — depression, feeling of increased anxiety.

From the side of musculoskeletal system: often — arthralgia, myalgia.

With the hematopoietic system: rarely — neutropenia, agranulocytosis, thrombocytopenia.

The immune system: often — urticaria, erythema multiforme rarely systemic allergic reactions (reactions similar to serum sickness, angioedema) very rarely — severe skin reaction (toxic epidermal necrolysis, Stevens-Johnson syndrome, photosensitivity). With the progression of skin rashes treatment terbinafine should be discontinued.

Other: often — headache, feeling sick, feeling tired very rarely, exacerbation of psoriasis, excessive hair loss.

Cream:

At the site of application, the redness, itching or burning allergic reactions.

Drug interactions:

Pills

Virtually no effect on the clearance of drugs metabolized by cytochrome P450 (e.g. cyclosporine, terfenadine, tolbutamide, triazolam, oral contraceptives).

Inhibits isoenzyme C?P2D6 and prevents the metabolism of drugs, such as tricyclic antidepressants and selective blockers of serotonin capture (e.g. desipramine, fluvoxamine), beta-blockers (metoprolol, propranolol), antiarrhythmic funds (flecainid, propafenon), MAO-b inhibitors (e.g. selegiline) and antipsychotic (e.g. chlorpromazine, haloperidol) funds. Drugs-???450 enzyme inducers (e.g. rifampicin) can accelerate the excretion of terbinafine from the body.

Drugs-SUR450 inhibitors (e.g. cimetidine) can slow metabolism and excretion of terbinafine from the body. While the use of these drugs may require adjustment of the dose of terbinafine.

Possible violation of the menstrual cycle while taking terbinafine and oral contraceptives.

Decreases the clearance of caffeine by 21% and prolongs its biological half-life by 31%.

Does not affect the clearance of antipyrine, digoxin, warfarin.

Ethanol and other hepatotoxic funds increase the risk of hepatotoxic effect.

Cream

Any drug interactions for Activin cream is not known.

Method of application and dose:

Inside, externally.

Inside. The duration of treatment and dosage regimen set individually and depend on the localization and severity of the disease.

Adults: the usual dose is 250 mg (1 table.) 1 time a day.

The onychomycosis: the duration of therapy is 6-12 weeks. If it affects the nails fingers and toes (except big toe), or at a young age the duration of treatment may be less than 12 weeks. An infection of the big toe 3-month course of treatment is usually sufficient. In rare cases, the slow rate of nail growth may require a longer treatment — up to 6 (or more) months.

Fungal skin infections: duration of treatment for interdigital, plantar or the type of "socks" localization of infection — 2-6 weeks in the mycoses of other parts of the body: calves — 2-4 weeks, body to 4 weeks in the mycoses caused by Candida, is 2-4 weeks in the athlete's head, caused by Microsporum canis — more than 4 weeks.

Children: normally — 125 mg (1/2 table).

Duration of treatment fungal infections of the scalp about 4 weeks, when infected by Microsporum canis may be longer.

Body weight <20 kg 62.5 mg (1/4 tabl.) 1 times per day 20 to 40 kg 125 mg (1/2 table.) 1 time per day >40 kg — 250 mg (1 table.) 1 time per day.

Elderly patients drug is prescribed in the same doses, as adults.

When expressed human liver and/or kidney (Cl creatinine <50 ml/min or concentration of creatinine in the blood >300 mkmol/l) — 125 mg 1 time per day.

Externally. Before applying the cream should be clean and dry affected areas. The cream is applied 1-2 times a day thin layer to the affected skin and surrounding areas and gently RUB. Infections accompanied by diaper rash (under Breasts, in the interdigital intervals, between the buttocks, in the inguinal region), place of applying the cream can be covered with gauze, especially at night.

The average duration of treatment

Ringworm of the body, legs: 1-2 weeks 1 time a day.

Ringworm of the feet: 2-4 weeks 1 time a day.

Candidiasis of the skin: 1-2 weeks 1 or 2 times a day.

Pityriasis versicolor: 2 weeks 1 or 2 times a day.

The decrease in the severity of clinical manifestations usually noted in the first days of treatment. In the case of irregular treatment or premature termination there is a risk of renewed infection. If after 1-2 weeks of treatment were observed signs of improvement, should conduct a verification of the diagnosis.

The elderly the dosage Azifine cream does not differ from that described above.

Children. Not recommended the use of this drug in children up to 12 years.

Overdose:

Symptoms: nausea, vomiting, pain in the lower abdomen, in the epigastric region.

Treatment: gastric lavage with subsequent appointment activated charcoal and/or symptomatic therapy.

The cases of drug overdose of the cream is not reported. If by chance Aktifin cream is ingested, can be expected to develop the same side effects as the overdose of tablets Azifine (headache, nausea, epigastric pain and dizziness).

Special instructions:

Terbinafine irregular use or premature discontinuation of treatment leads to relapse.

The duration of therapy can be affected by factors such as, for example, the presence of concomitant diseases, the condition of nails at the beginning of treatment.

If after 2 weeks of treatment skin infections there has been no improvement, you need to re-determine the causative agent and its sensitivity to the drug.

Systemic application in onychomycosis justified only in the case of total destruction of most of the nails, presence of a pronounced subungual hyperkeratosis, the ineffectiveness of the previous local therapy. In the treatment of onychomycosis clinical response, usually observed some months after mycological cure and cessation of treatment, due to the speed of regrowth of healthy nail. Removal of nail plates in treatment of onychomycosis of hands for 3 weeks and stop for onychomycosis 6 weeks is required.

In the presence of severe renal failure (Cl creatinine <50 ml/min or creatinine in the blood >300 mkmol/l), in violation of the liver dose of terbinafine should be halved.

In the presence of liver disease, the clearance of terbinafine can be reduced. With reduced liver function prescribed half the adult dose. During treatment should monitor the level transaminaz liver in serum. In rare cases, through 3 months of treatment occurs cholestasis and hepatitis. If signs of liver dysfunction (weakness, persistent nausea, loss of appetite, abdominal pain, jaundice, dark urine or colourless stool) the drug should be discontinued.

The appointment of terbinafine psoriasis patients require greater care, because in very rare cases, terbinafine may cause a psoriasis outbreak.

In the treatment of terbinafine should follow the General rules of hygiene to prevent reinfection through underwear and shoes. In the course of treatment (every 2 weeks) and at the end it is necessary to produce antifungal treatment of footwear, socks and stockings.

Effects on ability to drive and work mechanism: terbinafine does not affect the ability to drive and perform work requiring high concentration.

Aktifin cream is intended for external use only. Avoid getting it into eyes, as it may cause irritation. In case of contact with eyes, immediately wash out with running water, and in the case of persistent phenomena irritation, consult a doctor. With the development of allergic reactions should stop the drug.